PG 99-465 是一种高亲和力、选择性的 VPAC2 受体拮抗剂。该化合物对 VPAC1 受体显示出部分激动活性。
编号：200403
CAS号：2243219-86-3
单字母：Myristicacid-HSDAVFTDNYTKLRKQMAVKKYLNSIKKGGT-OH
| 编号: | 200403 |
| 中文名称: | 血管活性肠肽Myristoyl-(Lys12.27.28)-VIP-Gly-Gly-Thr (free acid) |
| 英文名: | Myristoyl-(Lys12.27.28)-VIP-Gly-Gly-Thr (free acid) |
| CAS号: | 2243219-86-3 |
| 单字母: | Myristicacid-HSDAVFTDNYTKLRKQMAVKKYLNSIKKGGT-OH |
| 三字母: | Myristicacid N端肉豆蔻酸修饰 -His组氨酸 -Ser丝氨酸 -Asp天冬氨酸 -Ala丙氨酸 -Val缬氨酸 -Phe苯丙氨酸 -Thr苏氨酸 -Asp天冬氨酸 -Asn天冬酰胺 -Tyr酪氨酸 -Thr苏氨酸 -Lys赖氨酸 -Leu亮氨酸 -Arg精氨酸 -Lys赖氨酸 -Gln谷氨酰胺 -Met甲硫氨酸 -Ala丙氨酸 -Val缬氨酸 -Lys赖氨酸 -Lys赖氨酸 -Tyr酪氨酸 -Leu亮氨酸 -Asn天冬酰胺 -Ser丝氨酸 -Ile异亮氨酸 -Lys赖氨酸 -Lys赖氨酸 -Gly甘氨酸 -Gly甘氨酸 -Thr苏氨酸 -OHC端羧基 |
| 氨基酸个数: | 31 |
| 分子式: | C171H283O47N45S1 |
| 平均分子量: | 3753.42 |
| 精确分子量: | 3751.09 |
| 等电点(PI): | 11.5 |
| pH=7.0时的净电荷数: | 7.24 |
| 平均亲水性: | 0.22413793103448 |
| 疏水性值: | -0.84 |
| 消光系数: | 2980 |
| 来源: | 人工化学合成，仅限科学研究使用，不得用于人体。 |
| 储存条件: | 负80℃至负20℃ |
| 标签: | 烷基化肽 血管活性肠肽 癌症研究肽 |
PG 99-465 is a high affinity, selective VPAC2 receptor antagonist. It exhibited a 100-fold preference for the VPAC2 over the VPAC1 receptor. The compound showed partial agonistic activity on the VPAC1 receptor and was inactive on the VPAC2 receptor transfected in CHO cells, as well as on naturally expressed human VPAC2 receptors in the SUP T1 cell line. Dickson et al. observed an agonistic effect of PG99-465 on the human VPAC1 and PAC1 receptors. When applied singly, PG99-465 increased [cAMP](i) at all three hVPAC/PAC receptor subtypes.
烷基化肽-说明
专肽生物可提供多肽烷基化修饰，增加多肽一端的疏水性，例如常见的C18，C16，C14，C12，以及C6等，也可根据客户要求，接其他长度的烷基化链。
化学预防肽是有助于预防疾病（例如癌症或糖尿病）的发作或发展的肽。这些肽可以源自天然来源，例如大豆或牛奶，也可以来自肽模拟物的设计，也可以源自使用合成肽进行的肽筛选。据认为，这些肽中的某些可以充当细胞周期的调节剂，其调节使细胞通过复制周期前进所需的蛋白质的产生和功能。另外，现在有越来越多的证据表明特定的饮食模式，食物和饮料以及其他饮食物质可以而且确实可以预防癌症。越来越多的流行病学研究表明，食物，营养和身体活动在预防和改变癌症过程中很重要。包括植物蛋白酶抑制剂，乳铁蛋白，乳铁蛋白，凝集素和lunasin在内的不同类型的食物蛋白和多肽似乎起着化学预防剂的作用。如今，蛋白质和多肽被认为是一组营养保健品，在预防癌症的不同阶段（包括起始，促进和进展）方面显示出潜力。此外，已经发现在植物中发现的一些蛋白酶抑制剂，例如豆类和大豆，是有效的癌发生抑制剂。致癌作用是引发和促进癌症的过程。 Bowman-Birk抑制剂和Kunitz胰蛋白酶抑制剂就在其中。目前，这些化合物在致癌作用中的生物学功能主要归因于抑制癌细胞的侵袭和转移，但是，其作用机理仍不完全清楚，需要进一步研究以充分阐明它们。
| DOI | 名称 | |
|---|---|---|
| 10.1046/j.1365-2826.2002.00826.x | Effects of vasoactive intestinal polypeptide on neurones of the rat suprachiasmatic nuclei in vitro | 下载 |
| 10.1046/j.1460-9568.2003.02425.x | The mouse VPAC2 receptor confers suprachiasmatic nuclei cellular rhythmicity and responsiveness to vasoactive intestinal polypeptide in vitro | 下载 |
| 10.1038/sj.bjp.0705918 | Inhibitory pathways in the circular muscle of rat jejunum | 下载 |
| 10.1016/j.brainres.2005.04.077 | VIP enhances synaptic transmission to hippocampal CA1 pyramidal cells through activation of both VPAC1 and VPAC2 receptors | 下载 |
| 10.1016/j.neuropharm.2006.07.017 | A systematic comparison of intracellular cyclic AMP and calcium signalling highlights complexities in human VPAC/PAC receptor pharmacology | 下载 |
| 10.1124/mol.109.060137 | Identification and characterization of a small molecule antagonist of human VPAC(2) receptor | 下载 |
| 10.1016/j.neuron.2013.06.026 | Translational control of entrainment and synchrony of the suprachiasmatic circadian clock by mTOR/4E-BP1 signaling | 下载 |
| 10.1002/syn.21772 | Augmented cystine-glutamate exchange by pituitary adenylate cyclase-activating polypeptide signaling via the VPAC1 receptor | 下载 |
| 10.1002/jez.1964 | Sex steroid hormone secretion in the wall lizard Podarcis sicula testis: The involvement of VIP | 下载 |
多肽Myristicacid-His-Ser-Asp-Ala-Val-Phe-Thr-Asp-Asn-Tyr-Thr-Lys-Leu-Arg-Lys-Gln-Met-Ala-Val-Lys-Lys-Tyr-Leu-Asn-Ser-Ile-Lys-Lys-Gly-Gly-Thr-COOH的合成步骤：
1、合成CTC树脂：称取2.16g CTC Resin（如初始取代度约为1.04mmol/g）和2.7mmol Fmoc-Thr(tBu)-OH于反应器中，加入适量DCM溶解氨基酸（需要注意，此时CTC树脂体积会增大好几倍，避免DCM溶液过少），再加入6.74mmol DIPEA（Mw：129.1,d：0.740g/ml），反应2-3小时后，可不抽滤溶液，直接加入1ml的HPLC级甲醇，封端半小时。依次用DMF洗涤2次，甲醇洗涤1次，DCM洗涤一次，甲醇洗涤一次，DCM洗涤一次，DMF洗涤2次（这里使用甲醇和DCM交替洗涤，是为了更好地去除其他溶质，有利于后续反应）。得到 Fmoc-Thr(tBu)-CTC Resin。结构图如下：
2、脱Fmoc：加3倍树脂体积的20%Pip/DMF溶液，鼓氮气30分钟，然后2倍树脂体积的DMF 洗涤5次。得到 H2N-Thr(tBu)-CTC Resin 。（此步骤脱除Fmoc基团，茚三酮检测为蓝色，Pip为哌啶）。结构图如下：
3、缩合：取6.74mmol Fmoc-Gly-OH 氨基酸，加入到上述树脂里，加适当DMF溶解氨基酸，再依次加入13.48mmol DIPEA，6.4mmol HBTU。反应30分钟后，取小样洗涤，茚三酮检测为无色。用2倍树脂体积的DMF 洗涤3次树脂。（洗涤树脂，去掉残留溶剂，为下一步反应做准备）。得到Fmoc-Gly-Thr(tBu)-CTC Resin。氨基酸：DIPEA：HBTU：树脂=3：6：2.85：1（摩尔比）。结构图如下：
4、依次循环步骤二、步骤三，依次得到
H2N-Gly-Thr(tBu)-CTC Resin
Fmoc-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Thr(tBu)-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Thr(tBu)-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Tyr(tBu)-Thr(tBu)-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Tyr(tBu)-Thr(tBu)-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Asn(Trt)-Tyr(tBu)-Thr(tBu)-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Asn(Trt)-Tyr(tBu)-Thr(tBu)-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Asp(OtBu)-Asn(Trt)-Tyr(tBu)-Thr(tBu)-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Asp(OtBu)-Asn(Trt)-Tyr(tBu)-Thr(tBu)-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Thr(tBu)-Asp(OtBu)-Asn(Trt)-Tyr(tBu)-Thr(tBu)-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Thr(tBu)-Asp(OtBu)-Asn(Trt)-Tyr(tBu)-Thr(tBu)-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Phe-Thr(tBu)-Asp(OtBu)-Asn(Trt)-Tyr(tBu)-Thr(tBu)-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Phe-Thr(tBu)-Asp(OtBu)-Asn(Trt)-Tyr(tBu)-Thr(tBu)-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Val-Phe-Thr(tBu)-Asp(OtBu)-Asn(Trt)-Tyr(tBu)-Thr(tBu)-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Val-Phe-Thr(tBu)-Asp(OtBu)-Asn(Trt)-Tyr(tBu)-Thr(tBu)-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Ala-Val-Phe-Thr(tBu)-Asp(OtBu)-Asn(Trt)-Tyr(tBu)-Thr(tBu)-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Ala-Val-Phe-Thr(tBu)-Asp(OtBu)-Asn(Trt)-Tyr(tBu)-Thr(tBu)-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Asp(OtBu)-Ala-Val-Phe-Thr(tBu)-Asp(OtBu)-Asn(Trt)-Tyr(tBu)-Thr(tBu)-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Asp(OtBu)-Ala-Val-Phe-Thr(tBu)-Asp(OtBu)-Asn(Trt)-Tyr(tBu)-Thr(tBu)-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-Ser(tBu)-Asp(OtBu)-Ala-Val-Phe-Thr(tBu)-Asp(OtBu)-Asn(Trt)-Tyr(tBu)-Thr(tBu)-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
H2N-Ser(tBu)-Asp(OtBu)-Ala-Val-Phe-Thr(tBu)-Asp(OtBu)-Asn(Trt)-Tyr(tBu)-Thr(tBu)-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
Fmoc-His(Trt)-Ser(tBu)-Asp(OtBu)-Ala-Val-Phe-Thr(tBu)-Asp(OtBu)-Asn(Trt)-Tyr(tBu)-Thr(tBu)-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin
以上中间结构，均可在专肽生物多肽计算器-多肽结构计算器中，一键画出。
最后再经过步骤二得到 H2N-His(Trt)-Ser(tBu)-Asp(OtBu)-Ala-Val-Phe-Thr(tBu)-Asp(OtBu)-Asn(Trt)-Tyr(tBu)-Thr(tBu)-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTC Resin，结构如下：
5、肉豆蔻酸反应连接：在上述树脂中，加入适当DMF后，再加入6.74mmol 肉豆蔻酸到树脂中，再加入13.48mmol DIPEA、6.4mmol HBTU，鼓氮气反应30分钟。用2倍树脂体积的DMF 洗涤3次树脂（洗涤树脂，去掉残留溶剂，为下一步反应做准备）。 得到Myristicacid-His(Trt)-Ser(tBu)-Asp(OtBu)-Ala-Val-Phe-Thr(tBu)-Asp(OtBu)-Asn(Trt)-Tyr(tBu)-Thr(tBu)-Lys(Boc)-Leu-Arg(Pbf)-Lys(Boc)-Gln(Trt)-Met-Ala-Val-Lys(Boc)-Lys(Boc)-Tyr(tBu)-Leu-Asn(Trt)-Ser(tBu)-Ile-Lys(Boc)-Lys(Boc)-Gly-Gly-Thr(tBu)-CTCResin。 结构如下：
6、切割：6倍树脂体积的切割液（或每1g树脂加8ml左右的切割液），摇床摇晃 2小时，过滤掉树脂，用冰无水乙醚沉淀滤液，并用冰无水乙醚洗涤沉淀物3次，最后将沉淀物放真空干燥釜中，常温干燥24小试，得到粗品Myristicacid-His-Ser-Asp-Ala-Val-Phe-Thr-Asp-Asn-Tyr-Thr-Lys-Leu-Arg-Lys-Gln-Met-Ala-Val-Lys-Lys-Tyr-Leu-Asn-Ser-Ile-Lys-Lys-Gly-Gly-Thr-COOH。结构图见产品结构图。
切割液选择：1）TFA：H2O=95%：5%
2）TFA：H2O：TIS=95%：2.5%：2.5%
3）三氟乙酸：茴香硫醚：1，2-乙二硫醇：苯酚：水=87.5%：5%：2.5%：2.5%：2.5%
（前两种适合没有容易氧化的氨基酸，例如Trp、Cys、Met。第三种适合几乎所有的序列。）
6、纯化冻干：使用液相色谱纯化，收集目标峰液体，进行冻干，获得蓬松的粉末状固体多肽。不过这时要取小样复测下纯度 是否目标纯度。
7、最后总结：
杭州专肽生物技术有限公司（ALLPEPTIDE https://www.allpeptide.com）主营定制多肽合成业务，提供各类长肽，短肽，环肽，提供各类修饰肽，如：荧光标记修饰（CY3、CY5、CY5.5、CY7、FAM、FITC、Rhodamine B、TAMRA等），功能基团修饰肽（叠氮、炔基、DBCO、DOTA、NOTA等），同位素标记肽（N15、C13），订书肽（Stapled Peptide）,脂肪酸修饰肽（Pal、Myr、Ste），磷酸化修饰肽（P-Ser、P-Thr、P-Tyr），环肽（酰胺键环肽、一对或者多对二硫键环），生物素标记肽，PEG修饰肽，甲基化修饰肽等。
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